Peringatan Keamanan

Symptoms of overdose and/or acute systemic toxicity involves central nervous system toxicity that presents with symptoms of increasing severity L5930. Patients may present initially with circumoral paraesthesia, numbness of the tongue, light-headedness, hyperacusis, and tinnitus L5930. Visual disturbance and muscular tremors or muscle twitching are more serious and precede the onset of generalized convulsions L5930. These signs must not be mistaken for neurotic behavior L5930. Unconsciousness and grand mal convulsions may follow, which may last from a few seconds to several minutes L5930. Hypoxia and hypercapnia occur rapidly following convulsions due to increased muscular activity, together with the interference with normal respiration and loss of the airway L5930. In severe cases, apnoea may occur. Acidosis increases the toxic effects of local anesthetics L5930. Effects on the cardiovascular system may be seen in severe cases L5930. Hypotension, bradycardia, arrhythmia and cardiac arrest may occur as a result of high systemic concentrations, with potentially fatal outcome L5930.

Pregnancy Category B has been established for the use of lidocaine in pregnancy, although there are no formal, adequate, and well-controlled studies in pregnant women F4349. General consideration should be given to this fact before administering lidocaine to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place F4349. Ultimately, although animal studies have revealed no evidence of harm to the fetus, lidocaine should not be administered during early pregnancy unless the benefits are considered to outweigh the risks L5930. Lidocaine readily crosses the placental barrier after epidural or intravenous administration to the mother L5930. The ratio of umbilical to maternal venous concentration is 0.5 to 0.6 L5930. The fetus appears to be capable of metabolizing lidocaine at term L5930. The elimination half-life in the newborn of the drug received in utero is about three hours, compared with 100 minutes in the adult L5930. Elevated lidocaine levels may persist in the newborn for at least 48 hours after delivery L5930. Fetal bradycardia or tachycardia, neonatal bradycardia, hypotonia or respiratory depression may occur L5930.

Local anesthetics rapidly cross the placenta and when used for epidural, paracervical, pudendal or caudal block anesthesia, can cause varying degrees of maternal, fetal and neonatal toxicity F4349. The potential for toxicity depends upon the procedure performed, the type and amount of drug used, and the technique of drug administration F4349. Adverse reactions in the parturient, fetus and neonate involve alterations of the central nervous system, peripheral vascular tone, and cardiac function F4349.

Maternal hypotension has resulted from regional anesthesia F4349. Local anesthetics produce vasodilation by blocking sympathetic nerves F4349. Elevating the patient’s legs and positioning her on her left side will help prevent decreases in blood pressure F4349. The fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable F4349.

Epidural, spinal, paracervical, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts F4349. In one study, paracervical block anesthesia was associated with a decrease in the mean duration of first stage labor and facilitation of cervical dilation F4349. However, spinal and epidural anesthesia have also been reported to prolong the second stage of labor by removing the parturient’s reflex urge to bear down or by interfering with motor function F4349. The use of obstetrical anesthesia may increase the need for forceps assistance F4349.

The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life F4349. The long-term significance of these observations is unknown F4349. Fetal bradycardia may occur in 20 to 30 percent of patients receiving paracervical nerve block anesthesia with the amide-type local anesthetics and may be associated with fetal acidosis F4349. Fetal heart rate should always be monitored during paracervical anesthesia F4349. The physician should weigh the possible advantages against risks when considering a paracervical block in prematurity, toxemia of pregnancy, and fetal distress F4349. Careful adherence to the recommended dosage is of the utmost importance in obstetrical paracervical block F4349. Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection F4349. Cases compatible with unintended fetal intracranial injection of local anesthetic solution have been reported following intended paracervical or pudendal block or both. Babies so affected present with unexplained neonatal depression at birth, which correlates with high local anesthetic serum levels, and often manifest seizures within six hours F4349. Prompt use of supportive measures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication F4349.

It is not known whether this drug is excreted in human milk F4349. Because many drugs are excreted in human milk, caution should be exercised when lidocaine is administered to a nursing woman F4349.

Dosages in children should be reduced, commensurate with age, body weight and physical condition F4349.

The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats F4349.

Lidocaine

DB00281

small molecule approved vet_approved

Deskripsi

Ever since its discovery and availability for sale and use in the late 1940s, lidocaine has become an exceptionally commonly used medication T583. In particular, lidocaine's principal mode of action in acting as a local anesthetic that numbs the sensations of tissues means the agent is indicated for facilitating local anesthesia for a large variety of surgical procedures F4349, L5930, L5948. It ultimately elicits its numbing activity by blocking sodium channels so that the neurons of local tissues that have the medication applied on are transiently incapable of signaling the brain regarding sensations F4349, L5930, L5948. In doing so, however, it can block or decrease muscle contractile, resulting in effects like vasodilation, hypotension, and irregular heart rate, among others F4349, L5930, L5948. As a result, lidocaine is also considered a class Ib anti-arrhythmic agent L5930, L5948, F4468. Nevertheless, lidocaine's local anesthetic action sees its use in many medical situations or circumstances that may benefit from its action, including the treatment of premature ejaculation A177625.

Regardless, lidocaine is currently available as a relatively non-expensive generic medication that is written for in millions of prescriptions internationally on a yearly basis. It is even included in the World Health Organization's List of Essential Medicines L6055.

Struktur Molekul 2D

Berat 234.3373
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of lidocaine hydrochloride following an intravenous bolus injection is typically 1.5 to 2.0 hours [F4349]. Because of the rapid rate at which lidocaine hydrochloride is metabolized, any condition that affects liver function may alter lidocaine HCl kinetics [F4349]. The half-life may be prolonged two-fold or more in patients with liver dysfunction [F4349].
Volume Distribusi The volume of distribution determined for lidocaine is 0.7 to 1.5 L/kg [L5948]. In particular, lidocaine is distributed throughout the total body water [L5930]. Its rate of disappearance from the blood can be described by a two or possibly even three-compartment model [L5930]. There is a rapid disappearance (alpha phase) which is believed to be related to uptake by rapidly equilibrating tissues (tissues with high vascular perfusion, for example) [L5930]. The slower phase is related to distribution to slowly equilibrating tissues (beta phase) and to its metabolism and excretion (gamma phase) [L5930]. Lidocaine's distribution is ultimately throughout all body tissues [L5930]. In general, the more highly perfused organs will show higher concentrations of the agent [L5930]. The highest percentage of this drug will be found in skeletal muscle, mainly due to the mass of muscle rather than an affinity [L5930].
Klirens (Clearance) The mean systemic clearance observed for intravenously administered lidocaine in a study of 15 adults was approximately 0.64 +/- 0.18 L/min [F4444].

Absorpsi

In general, lidocaine is readily absorbed across mucous membranes and damaged skin but poorly through intact skin F4468. The agent is quickly absorbed from the upper airway, tracheobronchial tree, and alveoli into the bloodstream F4468. And although lidocaine is also well absorbed across the gastrointestinal tract the oral bioavailability is only about 35% as a result of a high degree of first-pass metabolism F4468. After injection into tissues, lidocaine is also rapidly absorbed and the absorption rate is affected by both vascularity and the presence of tissue and fat capable of binding lidocaine in the particular tissues F4468. The concentration of lidocaine in the blood is subsequently affected by a variety of aspects, including its rate of absorption from the site of injection, the rate of tissue distribution, and the rate of metabolism and excretion F4349, L5930, L5948. Subsequently, the systemic absorption of lidocaine is determined by the site of injection, the dosage given, and its pharmacological profile F4349, L5930, L5948. The maximum blood concentration occurs following intercostal nerve blockade followed in order of decreasing concentration, the lumbar epidural space, brachial plexus site, and subcutaneous tissue F4349, L5930, L5948. The total dose injected regardless of the site is the primary determinant of the absorption rate and blood levels achieved F4349, L5930, L5948. There is a linear relationship between the amount of lidocaine injected and the resultant peak anesthetic blood levels F4349, L5930, L5948. Nevertheless, it has been observed that lidocaine hydrochloride is completely absorbed following parenteral administration, its rate of absorption depending also on lipid solubility and the presence or absence of a vasoconstrictor agent F4349, L5930, L5948. Except for intravascular administration, the highest blood levels are obtained following intercostal nerve block and the lowest after subcutaneous administration F4349, L5930, L5948. Additionally, lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion F4349.

Metabolisme

Lidocaine is metabolized predominantly and rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys F4349, L5930. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation F4349, L5930. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide F4349, L5930. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine HCl F4349, L5930. Approximately 90% of lidocaine HCl administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged F4349, L5930. The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-dimethylaniline F4349, L5930.

Rute Eliminasi

The excretion of unchanged lidocaine and its metabolites occurs predominantly via the kidney with less than 5% in the unchanged form appearing in the urine F4349, L5930. The renal clearance is inversely related to its protein binding affinity and the pH of the urine L5930. This suggests by the latter that excretion of lidocaine occurs by non-ionic diffusion L5930.

Interaksi Obat

2085 Data
Deferasirox The serum concentration of Lidocaine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Lidocaine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Lidocaine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Lidocaine can be decreased when it is combined with Teriflunomide.
Buprenorphine Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Hydrocodone Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Magnesium sulfate The therapeutic efficacy of Lidocaine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lidocaine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Mirtazapine Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Orphenadrine Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Pramipexole Lidocaine may increase the sedative activities of Pramipexole.
Rotigotine Lidocaine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Lidocaine.
Sodium oxybate Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Thalidomide Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amiodarone The risk or severity of generalized seizure and bradycardia can be increased when Amiodarone is combined with Lidocaine.
Hyaluronidase (ovine) Hyaluronidase (ovine) can cause an increase in the absorption of Lidocaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Hyaluronidase (human recombinant) Hyaluronidase (human recombinant) can cause an increase in the absorption of Lidocaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Hyaluronidase Hyaluronidase can cause an increase in the absorption of Lidocaine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Lidocaine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Lidocaine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Lidocaine.
Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Lidocaine.
Pirfenidone The metabolism of Pirfenidone can be decreased when combined with Lidocaine.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Lidocaine.
Mirabegron The serum concentration of Lidocaine can be increased when it is combined with Mirabegron.
Abiraterone The serum concentration of Lidocaine can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Lidocaine can be increased when combined with Cyproterone acetate.
Ethanol Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Lidocaine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.
Desvenlafaxine The serum concentration of Lidocaine can be increased when it is combined with Desvenlafaxine.
Sibutramine The risk or severity of adverse effects can be increased when Lidocaine is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Lidocaine is combined with Zimelidine.
Milnacipran The risk or severity of adverse effects can be increased when Lidocaine is combined with Milnacipran.
Indalpine The risk or severity of adverse effects can be increased when Lidocaine is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Lidocaine is combined with Alaproclate.
Esmolol The serum concentration of Lidocaine can be increased when it is combined with Esmolol.
Betaxolol The serum concentration of Lidocaine can be increased when it is combined with Betaxolol.
Metoprolol The serum concentration of Lidocaine can be increased when it is combined with Metoprolol.
Atenolol The serum concentration of Lidocaine can be increased when it is combined with Atenolol.
Timolol The serum concentration of Lidocaine can be increased when it is combined with Timolol.
Sotalol The serum concentration of Lidocaine can be increased when it is combined with Sotalol.
Labetalol The serum concentration of Lidocaine can be increased when it is combined with Labetalol.
Bisoprolol The serum concentration of Lidocaine can be increased when it is combined with Bisoprolol.
Alprenolol The serum concentration of Lidocaine can be increased when it is combined with Alprenolol.
Pindolol The serum concentration of Lidocaine can be increased when it is combined with Pindolol.
Carvedilol The serum concentration of Lidocaine can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Lidocaine can be increased when it is combined with Propafenone.
Acebutolol The serum concentration of Lidocaine can be increased when it is combined with Acebutolol.
Nadolol The serum concentration of Lidocaine can be increased when it is combined with Nadolol.
Bevantolol The serum concentration of Lidocaine can be increased when it is combined with Bevantolol.
Practolol The serum concentration of Lidocaine can be increased when it is combined with Practolol.
Penbutolol The serum concentration of Lidocaine can be increased when it is combined with Penbutolol.
Oxprenolol The serum concentration of Lidocaine can be increased when it is combined with Oxprenolol.
Dexpropranolol The serum concentration of Lidocaine can be increased when it is combined with Dexpropranolol.
Celiprolol The serum concentration of Lidocaine can be increased when it is combined with Celiprolol.
Nebivolol The serum concentration of Lidocaine can be increased when it is combined with Nebivolol.
Bufuralol The serum concentration of Lidocaine can be increased when it is combined with Bufuralol.
Bopindolol The serum concentration of Lidocaine can be increased when it is combined with Bopindolol.
Bupranolol The serum concentration of Lidocaine can be increased when it is combined with Bupranolol.
Indenolol The serum concentration of Lidocaine can be increased when it is combined with Indenolol.
Arotinolol The serum concentration of Lidocaine can be increased when it is combined with Arotinolol.
Levobetaxolol The serum concentration of Lidocaine can be increased when it is combined with Levobetaxolol.
Talinolol The serum concentration of Lidocaine can be increased when it is combined with Talinolol.
Anisodamine The serum concentration of Lidocaine can be increased when it is combined with Anisodamine.
Bucindolol The serum concentration of Lidocaine can be increased when it is combined with Bucindolol.
Esatenolol The serum concentration of Lidocaine can be increased when it is combined with Esatenolol.
Cloranolol The serum concentration of Lidocaine can be increased when it is combined with Cloranolol.
Mepindolol The serum concentration of Lidocaine can be increased when it is combined with Mepindolol.
Epanolol The serum concentration of Lidocaine can be increased when it is combined with Epanolol.
Tertatolol The serum concentration of Lidocaine can be increased when it is combined with Tertatolol.
Landiolol The serum concentration of Lidocaine can be increased when it is combined with Landiolol.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Lidocaine.
Ibutilide Lidocaine may increase the arrhythmogenic activities of Ibutilide.
Hyoscyamine Lidocaine may increase the arrhythmogenic activities of Hyoscyamine.
Acetyldigitoxin Lidocaine may increase the arrhythmogenic activities of Acetyldigitoxin.
Carteolol Lidocaine may increase the arrhythmogenic activities of Carteolol.
Atropine Lidocaine may increase the arrhythmogenic activities of Atropine.
Adenosine Lidocaine may increase the arrhythmogenic activities of Adenosine.
Moricizine Lidocaine may increase the arrhythmogenic activities of Moricizine.
Levosimendan Lidocaine may increase the arrhythmogenic activities of Levosimendan.
Deslanoside Lidocaine may increase the arrhythmogenic activities of Deslanoside.
Bretylium Lidocaine may increase the arrhythmogenic activities of Bretylium.
Metipranolol Lidocaine may increase the arrhythmogenic activities of Metipranolol.
Ajmaline Lidocaine may increase the arrhythmogenic activities of Ajmaline.
Azimilide Lidocaine may increase the arrhythmogenic activities of Azimilide.
Tedisamil Lidocaine may increase the arrhythmogenic activities of Tedisamil.

Target Protein

Sodium channel protein type 11 subunit alpha SCN11A
Sodium channel protein type 10 subunit alpha SCN10A
Sodium channel protein type 9 subunit alpha SCN9A
Sodium channel protein type 5 subunit alpha SCN5A
Epidermal growth factor receptor EGFR
Sodium channel protein type 4 subunit alpha SCN4A
Alpha-1-acid glycoprotein 1 ORM1
Alpha-1-acid glycoprotein 2 ORM2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17443559
    Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846.
  • PMID: 4694036
    Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508.
  • PMID: 17067740
    Geha PY, Baliki MN, Chialvo DR, Harden RN, Paice JA, Apkarian AV: Brain activity for spontaneous pain of postherpetic neuralgia and its modulation by lidocaine patch therapy. Pain. 2007 Mar;128(1-2):88-100. Epub 2006 Oct 25.
  • PMID: 15099246
    Hines R, Keaney D, Moskowitz MH, Prakken S: Use of lidocaine patch 5% for chronic low back pain: a report of four cases. Pain Med. 2002 Dec;3(4):361-5.
  • PMID: 28408390
    Authors unspecified: Lidocaine/prilocaine spray for premature ejaculation. Drug Ther Bull. 2017 Apr;55(4):45-48. doi: 10.1136/dtb.2017.4.0469.
Textbook
  • ISBN: 9780941901215
    Scriabine, Alexander (2017). Pharmaceutical Innovation: Revolutionizing Human Health.. Chemical Heritage Press..

Contoh Produk & Brand

Produk: 3729 • International brands: 16
Produk
  • 0.4% Lidocaine Hydrochloride and 5% Dextrose Injection
    Solution • - • Intravenous • Canada • Approved
  • 0.4% Lidocaine Hydrochloride and 5% Dextrose Injection USP
    Solution • - • Intravenous • Canada • Approved
  • 0.5% LIDOCAINE HCl
    Injection, solution • 5 mg/1mL • Infiltration; Intravenous • US • Generic • Approved
  • 1% Lidocaine Hci
    Injection, solution • 10 mg/1mL • Infiltration; Perineural • US • Generic • Approved
  • 1% Lidocaine Hci
    Injection, solution • 10 mg/1mL • Infiltration; Perineural • US • Generic • Approved
  • 10 Person ANSI
    Kit • - • Ophthalmic; Oral; Topical • US • OTC
  • 1st Medxpatch With Lidocaine 4%
    Patch • - • Topical • US • OTC
  • 1st Medxpatch With Lidocaine 4%-rx
    Patch • - • Topical • US
Menampilkan 8 dari 3729 produk.
International Brands
  • After Burn Double Strength Gel
  • After Burn Double Strength Spray
  • After Burn Gel
  • After Burn Spray
  • Alphacaine
  • Anestacon Jelly
  • DermaFlex
  • Dilocaine
  • Esracaine
  • L-Caine

Sekuens Gen/Protein (FASTA)

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